Treatment of acute and chronic colitis
Olsalazine sodium is a drug developed by Pharmacia A B Co., Switzerland, to treat acute and chronic colitis. It was first listed in Denmark in 1989. It has been collected and recordedby the European Pharmacopoeia 7 edition and the national drug standard WS1(X-349) -2004Z. Orsalazine sodium is a precursor drug consisting of two azo bonds linked to 5amino salicylic acid. The bacteria in the colon break up the diazo bond and release 5amino salicylic acid. 5amino salicylic acid acts on colitis mucosa, inhibits the formation of prostaglandins, leukotrienes and other inflammatory factors, and reduces membrane permeability, and plays a role in the treatment of ulcerative colitis. This product weakens the absorption of nitrogen, sodium and water in the ileum and colonic mucosa, which is transformed into secretion in human body. Patients with ulcerative colitis take 1g daily, and the whole intestinal transit time is shortened by 40%. If the healthy subjects are given oral administration of 2g once, It has no effect on the complex frequency of migration of the small intestine. But it can cause diarrhea in 30% of the users and increase the diarrhea of the patients with intestinal inflammation. The bioavailability of the whole body is extremely low. The absorption rate of the oral dose is less than 5%.
After absorption, about 10% doses will be conjugated to orsalazine sulfate, t1/2 about 1H and conjugated half life is about 7 days.
Figure 1 The structural formula of oralalazine sodium
Adverse reaction
The most common side effect is diarrhoea, the incidence of which is 17%. Usually, the difference between diarrhea and intestinal inflammation is that the excreta has high water content without blood, and is related to the dosage. It usually occurs when the treatment begins or the dose increases. Reduction the dose of this product or combined use with Loperamide, diarrhea will be controlled. Other side effects include headache, nausea, abdominal pain, rash, dizziness and joint pain. Most of the patients who are allergic or intolerant to sulfasalazine are resistant to this product. The male sterility treated with sulfasalazine improved after using this product.
Chemical Properties
Yellow Crystalline Powder
Uses
Mordant dye for wool.
Uses
Dimer of Mesalazine (M258100), an anti-inflammatory drug used in the treatment of inflammatory bowel disease and ulcerative colitis.
Uses
Dimer of Mesalamine. It is an anti-inflammatorydrug used in the treatment of inflammatory bowel disease and ulcerative colitis
Preparation
5-Amino-2-chlorobenzoic acid diazotization, coupled with 2-Hydroxybenzoic acid, and then in a certain pressure and contains trace copper powder or Cupric oxide of Sodium hydroxide solution common heating (130 ~ 150 ℃).
Definition
ChEBI: An organic sodium salt that is the disodium salt of 3,3'-azobis(6-hydroxybenzoic acid) (olsalazine). Effective in the treatment of inflammatory bowel disease and ulcerative colitis. Mechanism of action unknown, but appears to be topical
brand name
Dipentum (UCB).
Biological Activity
Olsalazine is an anti-inflammatory drug used in inflammatory bowel disease and ulcerative colitis treatments. It is a pro-drug of 5-aminosalicylic acid (mesalamine) th at it is converted by the bacteria in the colon to mesalamine. Olsalazine (5-aminosalicylic acid) is consider as a broad-spectrum anticancer agent. Additionally, olsalazine increases both eEF1A2 and utrophin A levels in in C2C12 myoblasts (relevant to Duchenne muscular dystrophy).
Clinical Use
Induction and maintenance of remission in ulcerative
colitis
Metabolism
Olsalazine is broken down by the colonic bacterial flora
into 2 molecules of 5-aminosalicylic acid (mesalazine).
The small amounts (1-2% of the dose or less) of intact
olsalazine that are absorbed are excreted mainly in urine.
Approximately 0.1% of an oral dose of olsalazine
is hepatically metabolised to olsalazine-O-sulfate
(olsalazine-S), which has a half-life of 7 days.
Properties and Applications
deep green light yellow. Soluble in water for green light yellow, moderate soluble in Etanol for green yellow. In concentrated sulfuric acid for yellow orange, dilution after light yellow, In concentrated nitric acid to red. Dye aqueous solution to join concentrated hydrochloric acid color greatly shallow for yellow; Join concentrated Sodium hydroxide solution for golden orange.
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Standard
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Ironing Fastness
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Light Fastness
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Fulling
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Persperation Fastness
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Soaping
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Water
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Alkali
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Acid
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ISO
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4-5
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6
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4-5
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2-3
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4-5
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5
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5
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AATCC
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5
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6-7
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4
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5
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5
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5
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